| Description | Clindamycin (Sobelin) dissociates peptidyl-tRNA from the bacterial ribosome, thereby disrupting bacterial protein synthesis. Clindamycin is a semisynthetic broad-spectrum antibiotic produced by chemical modification of the parent compound lincomycin. |
| In vitro | Clindamycin 是 lincomycin 的半合成类似物。它主要通过破坏酶催化的肽链合成启动来抑制肽链的合成。Clindamycin 对某些哺乳动物细胞的蛋白质合成有适度影响。[1] Clindamycin 对大多数革兰氏阳性需氧菌有效。与 lincomycin 相比，Clindamycin 对 Staphylococcus aureus 和 Streptococcus pneumonia 的活性约高出八倍。Clindamycin 的活性是 erythromycin 对 S. aureus 的四倍，并且即便是对 erythromycin、penicillin 和 methicillin 抵抗的菌株也有效。Clindamycin 对革兰氏阳性厌氧菌有效，对 Bacteroides 属菌高度活跃。[2] Clindamycin 还能够改变细菌表面，从而大大促进细菌的吞噬和细胞内杀菌。Clindamycin 增强了虹吸作用和吞噬作用。[4] |
| In vivo | Clindamycin（每日经肌肉注射50 mg/kg）可将对青霉素抗性的S. aureu感染的猴子的存活率提高到87.5%（7/8）。[5] Clindamycin（每天三次，每次40 mg/kg，经肌肉注射）能使87.5%（7/8）的兔子免受由B. fragillis、Streptococcus morbillorm、Fusobacterium nucleatum和Eubacterium lentum的混合物通过气管内接种引起的厌氧肺部感染。[6] Clindamycin（通过饮食混合给药，400 mg/kg）能将Toxoplasma gondii感染的小鼠的存活率提高到100%，而未经治疗的动物组全部死亡。[7] |
| Synonyms | Clinimycin, Sobelin, Chlolincocin, 克林霉素 |
| molecular weight | 424.98 |
| Molecular formula | C18H33ClN2O5S |
| CAS | 18323-44-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (105.89 mM), Sonication is recommended. Ethanol: 79 mg/mL (185.9 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Keusch GT, et al. J Infect Dis, 1976, 133(5), 578-587. 2. Dhawan VK, et al. Rev Infect Dis, 1982, 4(6), 1133-1153. 3. Carlisle HN, et al. Appl Microbiol, 1971, 21(3), 440-446. 4. Gemmell CG, et al. J Clin Invest, 1981, 67(5), 1249-1256. 5. McGehee RF Jr, et al. Am J Med Sci, 1968, 256(5), 279-292. 6. Hodille E, et al. Clindamycin suppresses virulence expression in inducible clindamycin-resistant Staphylococcus aureus strains. Ann Clin Microbiol Antimicrob. 2018 Oct 20;17(1):38. |